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Submit ReviewLSN 3318839 最新
说明： Glucagon-like peptide-1 receptor (GLP1-R) positive allosteric modulator
化学名： (R)-2-(2-(1-((R)-1-(2,6-Dichloro-3-cyclopropylphenyl)ethyl)-1H-imidazo[4,5-c]pyridin-6-yl)phenyl)propanoic acid
纯度： ≥98% (HPLC)
生物活性 for LSN 3318839
LSN 3318839 is a potent glucagon-like peptide-1 receptor (GLP1-R) positive allosteric modulator (EC50 = 14 nM). Acts as a molecular glue to stabilize peptide ligand and GLP1 receptor interaction. Potentiates activity of GLP-1 (7-36) (Cat. No. 2082) and the low-affinity metabolite GLP-1 (9-36) (Cat. No. 3266). LSN 3318839 alone or in combination with Sitagliptin (Cat. No. 6816) lowers glucose levels in animal models of diabetes. LSN 3318839 is orally bioavailable.
技术数据 for LSN 3318839
| 分子量 | 480.39 |
| 公式 | C26H23Cl2N3O2 |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 2764704-18-7 |
| PubChem ID | 162641136 |
| InChI Key | JPJWHCNGSBCZMI-HUUCEWRRSA-N |
| Smiles | C[C@H](C1=C(C(C2CC2)=CC=C1Cl)Cl)N3C4=CC(C5=C(C=CC=C5)[C@@H](C)C(O)=O)=NC=C4N=C3 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for LSN 3318839
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 48.04 | 100 |
制备储备液 for LSN 3318839
以下数据基于产品分子量 480.39。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.08 mL | 10.41 mL | 20.82 mL |
| 5 mM | 0.42 mL | 2.08 mL | 4.16 mL |
| 10 mM | 0.21 mL | 1.04 mL | 2.08 mL |
| 50 mM | 0.04 mL | 0.21 mL | 0.42 mL |
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产品说明书 for LSN 3318839
参考文献 for LSN 3318839
参考文献是支持产品生物活性的出版物。
Willard et al (2021) Discovery of an orally efficacious positive allosteric modulator of the glucagon-like peptide-1 receptor. J.Med.Chem. 64 3439 PMID: 33721487
If you know of a relevant reference for LSN 3318839, please let us know.
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关键词: LSN 3318839, LSN 3318839 supplier, LSN3318839, GLP-1R, Glucagon-like, Peptide-1, Receptor, potent, agonist, orally, bioavailable, sitagliptin, diabetes, Glucagon-Like, Peptide, 1, Receptors, 7959, Tocris Bioscience
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Peptides Involved in Appetite Modulation Scientific Review
Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and compounds available from Tocris are listed.